Anti-Trichomonas vaginalis activity of ursolic acid derivative: a promising alternative

• Published in: Parasitology research (1987) 2018-05, Vol.117 (5), p.1573-1580
• Main Authors: Bitencourt, Fernanda Gobbi, de Brum Vieira, Patrícia, Meirelles, Lucia Collares, Rigo, Graziela Vargas, da Silva, Elenilson Figueiredo, Gnoatto, Simone Cristina Baggio, Tasca, Tiana
• Format: Article
• Language: English
• Subjects: Animals; Antitrichomonal Agents - pharmacology; Biomedical and Life Sciences; Biomedicine; Cell Death - drug effects; Cell Line, Tumor; Cell lineage; Chlorocebus aethiops; Clinical isolates; Condoms; Cytotoxicity; Drug Resistance; Drug Synergism; Drug Therapy, Combination; Epithelium; Female; Health aspects; HeLa Cells; Hemolysis - drug effects; Humans; Immunology; Medical Microbiology; Metronidazole; Metronidazole - pharmacology; Microbial Sensitivity Tests; Microbiology; Minimum inhibitory concentration; Nitroimidazole; Original Paper; Parasitic diseases; Prevention; Sexually transmitted diseases; STD; Terpenoids; Trichomonas; Trichomonas Infections - drug therapy; Trichomonas Infections - parasitology; Trichomonas vaginalis; Trichomonas vaginalis - drug effects; Trichomonas Vaginitis - drug therapy; Trichomonas Vaginitis - parasitology; Trichomoniasis; Triterpenes - chemistry; Triterpenes - pharmacology; Ursolic Acid; Vero Cells
• ISSN: 0932-0113; 1432-1955
• DOI: 10.1007/s00436-018-5839-1

Trichomonas vaginalis is an extracellular parasite that binds to the epithelium of the human urogenital tract and causes the sexually transmitted infection, trichomoniasis. In view of increased resistance to drugs belonging to the 5-nitroimidazole class, new treatment alternatives are urgently needed. In this study, eight semisynthetized triterpene derivatives were evaluated for in vitro anti- T. vaginalis activity. Ursolic acid and its derivative, 3-oxime-urs-12-en-28-oic-ursolic acid ( 9 ), presented the best anti- T. vaginalis activity when compared to other derivatives, with minimum inhibitory concentration (MIC) at 25 μM. Moreover, 9 was active against several T. vaginalis fresh clinical isolates. Hemolysis assay demonstrated that 9 presented a low hemolytic effect. Importantly, 25 μM 9 was not cytotoxic against the Vero cell lineage. Finally, we demonstrated that compound 9 acts synergistically with metronidazole against a T. vaginalis metronidazole-resistant isolate. This report reveals the high potential of the triterpenoid derivative 9 as trichomonicidal agent.